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Alkyne compounds as well as preparation method and application thereof

A technology of alkyne compounds and compounds, which is applied in the field of extraction of alkyne compounds and active ingredients of traditional Chinese medicine, and can solve the problems of no activity or toxicity of other compounds

Active Publication Date: 2016-06-08
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, relevant researchers have extracted and isolated 17 polyacetylenic compounds from plants of the genus Bupleurum, among which Bupleurum toxin and acetylbupleurum toxin have significant neurotoxicity and cytotoxicity, and other compounds have no activity or reports of toxicity

Method used

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  • Alkyne compounds as well as preparation method and application thereof
  • Alkyne compounds as well as preparation method and application thereof
  • Alkyne compounds as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: the preparation of alkyne compound

[0021] (1) Preparation of Bupleurum Petroleum Ether

[0022] 5 kg of Bupleurum medicinal material was soaked in 95% ethanol for 12 hours, refluxed three times for 2 hours each time, the combined extracts were concentrated to obtain extract, and the extract was extracted with petroleum ether to obtain 150 g of Bupleurum petroleum ether fraction.

[0023] (2) Coarse separation of Bupleurum petroleum ether

[0024] Add the above-mentioned Bupleurum petroleum ether fraction sample to a silica gel chromatography column, use petroleum ether-ethyl acetate as the elution system, and sequentially use petroleum ether: ethyl acetate ratio of 100:0-0:100 for gradient elution. Silicone GF 254 Thin-layer chromatography plate and petroleum ether-ethyl acetate are used to develop the system to detect fractions. When the components monitored by thin-layer chromatography change significantly, replace the elution gradient with the next ...

Embodiment 2

[0077] Embodiment 2: Determination of in vitro activity of alkyne compounds

[0078] In vitro 5-HT, NA and DA monoamine transmitter reuptake inhibition tests were carried out on the compounds extracted and separated above.

[0079] 1. Source of experimental materials

[0080] ①Animals

[0081] Male SD rats were purchased from Shanghai Slack Experimental Animal Co., Ltd., body weight: 200-220g, animal certificate number: SCXK (Shanghai) 2012-0002, breeding room level: SPF level animal room for routine feeding.

[0082] ②Reference substance

[0083] Fluoxetine hydrochloride was purchased from the Chemical Division of Shanghai Pharmaceutical Industry Research Institute, desipramine was purchased from Sigma Company, and 6-hydroxydopamine was purchased from Sigma Company.

[0084] 2. Experimental material preparation

[0085] ① Preparation of test samples

[0086] I. Preparation of compounds

[0087] Compounds I, II, III and / or IV were respectively dissolved in 10% DMSO (dime...

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Abstract

The invention provides alkyne compounds as well as a preparation method and an application thereof and belongs to the technical field of extraction of alkyne compounds and effective ingredients of traditional Chinese medicines. Specifically, new compounds I, II and IV as well as a reported compound III are obtained from dried roots of Umbeliferae Bupleurum Radix Bupleuri through extraction and separation. In-vitro monoamine neurotransmitter reuptake inhibition experiments are conducted on the compounds, results indicate that the compounds I, II, III and IV have inhibition effects on reuptake of NA (noradrenaline), have the inhibition effects equivalent to that of positive control drug desipramine and have different degrees of inhibition effects on reuptake of 5-HT (5-hydroxytryptophan). The four compounds have anti-depression activity and are expected to be developed into drugs or prodrugs for preventing and treating anti-depression related diseases.

Description

technical field [0001] The invention relates to the technical field of extraction of acetylenic compounds and active ingredients of traditional Chinese medicines, in particular to an acetylenic compound, a method for separating the acetylenic compound from Bupleurum bupleuri, and the use of the acetylenic compound. Background technique [0002] Depression is a common mental illness characterized by high morbidity, relapse and disabling rates. Modern medical research shows that the pathogenesis of depression is complex, with many causes and various clinical symptoms. Most experts and scholars believe that the monoamine hypothesis of depression is that depression is caused by the deficiency of monoamine neurotransmitters in the human brain, 5-HT, NA or DA. The main antidepressants currently used clinically increase the concentration of monoamine transmitters in the synaptic cleft by inhibiting the reuptake of 5-HT and NA in the synaptic cleft. However, synthetic antidepressa...

Claims

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Application Information

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IPC IPC(8): C07C33/048C07C69/145C07C29/74C07C29/86C07C29/76C07C67/48C07C67/56C07C67/58A61K31/045A61K31/22A61P25/24
CPCC07C29/74C07C29/76C07C29/86C07C33/048C07C67/48C07C67/56C07C67/58C07C69/145
Inventor 高晓霞周玉枝方媛张峰秦雪梅张丽增
Owner SHANXI UNIV
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